Novel platinum(II) complexes of long chain aliphatic diamine ligands with oxalato as the leaving group: comparative cytotoxic activity relative to chloride precursors

Journal of the Brazilian Chemical Society

Universidade Federal de Minas Gerais, Belo Horizonte, Brazil¹  Silva, Heveline¹  Universidade Federal de Juiz de Fora, Juiz de Fora, Brazil¹  Fontes, Ana Paula S.¹  Frézard, Frederic¹  Departamento de Fisiologia e Biofísica¹  Rocha, Fillipe V.¹  Lopes, Miriam T. P.¹  Barra, Carolina V.¹ 

关键词: ethylenediamine;    oxalato;    platinum complexes;    antitumor agents;   

DOI  :  10.1590/S0103-50532010001000023

学科分类：化学（综合）

来源: SciELO

【 摘 要 】

Platinum complexes play an important role in the development of anticancer drugs. Their cytotoxicity can be influenced by the nature of the leaving ligands, due to the hydrolysis reaction that occurs prior to the binding of the platinum complex to DNA. Also, non-leaving groups such as lipophilic diamines may affect cellular uptake. In this work, we describe the synthesis of platinum(II) complexes having oxalato and long chain aliphatic N-alkyl ethylenediamines as ligands. The products were characterized by elemental analyses, infrared spectroscopy and 1H, 13C and 195Pt NMR spectroscopy. Biological activity was assessed against tumor cell lines (A549, B16-F1, B16-F10, MDA-MB-231) and non-tumor cell lines (BHK-21 and CHO). The length of the carbon chain affects the cytotoxicity and the oxalato complexes were less cytotoxic than the respective chloride-containing analogues.

【 授权许可】

Unknown